KU-0063794

For research use only. Not for use in humans.

製品コードS1226

KU-0063794化学構造

分子量(MW):465.54

KU-0063794 is a potent and highly specific dual-mTOR inhibitor of mTORC1 and mTORC2 with IC50 of ~10 nM in cell-free assays; no effect on PI3Ks.

サイズ 価格(税別) 在庫  
10mM (1mL in DMSO) JPY 31800 あり
JPY 16900 あり
JPY 30200 あり
JPY 80000 あり
JPY 113200 あり
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バルク問合せ

文献中Selleckの製品使用例(48)

製品安全説明書

mTOR阻害剤の選択性比較

生物活性

製品説明 KU-0063794 is a potent and highly specific dual-mTOR inhibitor of mTORC1 and mTORC2 with IC50 of ~10 nM in cell-free assays; no effect on PI3Ks.
ターゲット
mTORC1 [1]
(Cell-free assay)
mTORC2 [1]
(Cell-free assay)
~10 nM ~10 nM
体外試験

Compared with the mTOR inhibitor PP242, KU-0063794 exhibits higher specificity for mTOR, as being inactive against PI3Ks or 76 other kinases. In HEK-293 cells, KU-0063794 at 30 nM is sufficient to rapidly ablate S6K1 activity by blocking the phosphorylation of the hydrophobic motif (Thr389) and subsequently the phosphorylation of the T-loop residue (Thr229). In case of IGF1 stimulation of serum-starved HEK-293 cells, 300 nM of KU-0063794 is needed to inhibit the S6K1 activity by ~90%. KU-0063794 at 100-300 nM also completely inhibits the amino-acid-induced phosphorylation of S6K1 and S6 protein. Similar to S6K1, KU-0063794 inhibits the phosphorylation of mTORC1 at Ser2448 and mTORC2 at Ser2481 in a dose-dependent and time-dependent manner. In the presence of serum or following IGF1 stimulation, KU-0063794 induces a dose-dependent inhibition of the activity and phosphorylation of Akt at Ser473 and unexpected Thr308 as well as the phosphorylation of the Akt substrates PRAS40 at Thr246, GSK3α/GSK3β at Ser21/Ser9 and Foxo-1/3a at Thr24/Thr32. KU-0063794 but not rapamycin inhibits SGK1 activity and Ser422 phosphorylation as well as its physiological substrate NDGR1 in a dose-dependent manner, to the same extent as S6K1 and Akt phosphorylation, whereas KU-0063794 dose not inhibit phorbol ester induced ERK or RSK phosphorylation and RSK activation. Compared with rapamycin, KU-0063794 exhibits more significant potency to induce the complete dephosphorylation of 4E-BP1 at Thr37, Thr46 and Ser65. KU-0063794 inhibits cell growth of both wild-type and mLST8-deficient MEFs and induces a G1 cell cycle arrest, more significantly than rapamycin. [1]

細胞データ
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
HepG2  NV;DN29RS2WubDDWbYFjcWyrdImgRZN{[Xl? MnKxNE4y6oDVNUFCpO69VQ>? MYS3NkBp NXzmOVFQ\GWlcnXhd4V{KGOnbHygeoli[mmuaYT5JIlvKGFiZH;z[UBl\XCnbnTlcpQhdWGwbnXy NH\weoIzPjJ5OEixPS=>
HepG2  NF[2PHREd2yxbomgSo9zdWG2aX;uJGF{e2G7 NUSyb5JIOeLCk{WwxsDPxE1? NGDR[YUyOCCm M4fBOoRm[3KnYYPld{B1cGViboXtZoVzKG:oII\pZYJt\SCKZYDHNkBkd2yxbnnld:Khe2mpbnnmbYNidnSueR?= NGHtclgzPjJ5OEixPS=>
HepG2  NWewT3V2SXCxcITvd4l{KEG|c3H5 MUCwMlHjiJN3MNMg{txO Mmi1OFghcA>? M2K2Oolv\HWlZYOgZZBweHSxc3nzJIlvKGFiZH;z[UBl\XCnbnTlcpQhdWGwbnXy NFG5NJUzPjJ5OEixPS=>
HepG2  MUjGeY5kfGmxbjDBd5NigQ>? NF6xelk2NzFyIN88US=> MUCyOEBp NVPS[GJJ\HKjbXH0bYNidGy7IHnubIljcXS|IIDoc5NxcG:{eXzheIlwdiCxZjDBT3Qh[XRiU3XyMVQ4Ow>? M2jESlI3Ojd6OEG5
HepG2  MXrGeY5kfGmxbjDBd5NigQ>? NV72W|NJPS9zMDFOwG0> NHn6V2szPCCq NFTIWYZld3ewcnXneYxifGW|IITo[UBt\X[nbIOgTGlHOc7zIHHu[EBkgWOuaX6gSFHDqA>? MofGNlYzPzh6MUm=
HepG2  NICzTlFHfW6ldHnvckBCe3OjeR?= NVfBOHB{OC5z4pETOVDDqM7:TR?= NVHpSpVLOjRiaB?= M33SUIlv\HWlZYOgdFYzKGSxd37y[Yd2dGG2aX;uMEBD\WOuaX6tNUBmgHC{ZYPzbY9vKGGwZDDMR|NDNUlidH:gUGM{Si2LSTDjc453\XK|aX;uJIlvKGFiZH;z[UBl\XCnbnTlcpQhdWGwbnXy NGPXNIMzPjJ5OEixPS=>
HepG3  NHrRRnRHfW6ldHnvckBCe3OjeR?= MlPrNE4y6oDVNUFCpO69VQ>? MXG0PEBp MnTUbY5lfWOnczDj[YxtKGG3dH;wbIFogSCrbjDhJIRwe2ViZHXw[Y5l\W62IH3hco5meg>? M1vkNVI3Ojd6OEG5
AGS M2Lufmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUHDWmt1UUN3ME2xOU4xKMLzIEKuPVEh|ryP M{DON|I1PTl5NEe4
HGC27 M2HkfGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4GxfmlEPTB;MUWuNEDDuSB2LkiyJO69VQ>? Mo\aNlQ2QTd2N{i=
MKN45 M4rrV2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1XTUmlEPTB;MD64NkDDuSByLkCxJO69VQ>? NIW1WlYzPDV7N{S3PC=>
NUGC4 M3\CcGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVjJR|UxRTJwOUOgxtEhOC5|MTFOwG0> M17vUVI1PTl5NEe4
PC9 MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1\ERlczKGh? MnHFTWM2OD1zMD6xOeKyOC54MjDuUS=> M{XoVlI{QDd2OEiw
PC9GR MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3vGUFczKGh? NHTPOnRKSzVyPU[uNlHDuTFwM{Cgcm0> M{fofVI{QDd2OEiw
H1650 NGHrXWdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3nrd|czKGh? NWT6XIdvUUN3ME23MlYyyrFyLk[yJI5O NFnWNWEzOzh5NEi4NC=>
H1975 NVf2WpJJT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHHYT|c4OiCq NEX6cZFKSzVyPUGxMlE2yrFyLkmzJI5O M4LUUVI{QDd2OEiw
PC9 MVnGeY5kfGmxbjDBd5NigQ>? NHPaT4QyOC5zNTDuUS=> NWHiUHBsPzJiaB?= M4S0NYlvcGmkaYTzJI1VV1JicHjvd5Bpd3K7bHH0bY9vKHO2YYT1d:Kh MoP1NlM5PzR6OEC=
PC9GR MYXGeY5kfGmxbjDBd5NigQ>? NUW2R|FJPi5{MTDuUS=> NWLWbo11PzJiaB?= M{PTTIlvcGmkaYTzJI1VV1JicHjvd5Bpd3K7bHH0bY9vKHO2YYT1d:Kh M1vlPVI{QDd2OEiw
H1650 M3LGV2Z2dmO2aX;uJGF{e2G7 MX23MlYyKG6P MoP0O|IhcA>? NXf5RYF{cW6qaXLpeJMhdVSRUjDwbI9{eGixconsZZRqd25ic4TheJV{yqB? M4DHflI{QDd2OEiw
H1975 MYrGeY5kfGmxbjDBd5NigQ>? M2jTblEyNjF3IH7N M1S5N|czKGh? NGfFOpJqdmirYnn0d{BuXE:UIIDoc5NxcG:{eXzheIlwdiC|dHH0eZPDqA>? NILqVnAzOzh5NEi4NC=>
PC9 NEX0fGxHfW6ldHnvckBCe3OjeR?= NUjvfJFbOTBwMUWgcm0> Mlz1O|IhcA>? NY\zZnVocW6qaXLpeJMheGixc4Doc5J6dGG2aX;uJI9nKHB5MGO2Ty=> M{X1S|I{QDd2OEiw
PC9GR NFHRcJFHfW6ldHnvckBCe3OjeR?= NUTqc21TPi5{MTDuUS=> M2rTflczKGh? NXPIU2xbcW6qaXLpeJMheGixc4Doc5J6dGG2aX;uJI9nKHB5MGO2Ty=> MlHxNlM5PzR6OEC=
H1650 NG\telhHfW6ldHnvckBCe3OjeR?= NXq4[Io5Py54MTDuUS=> NFnke3k4OiCq Mo\UbY5pcWKrdIOgdIhwe3Cqb4L5cIF1cW:wIH;mJJA4OFN4Sx?= MVuyN|g4PDh6MB?=
H1975 MWfGeY5kfGmxbjDBd5NigQ>? MoKxNVEvOTVibl2= NVzTToI{PzJiaB?= NFjkS|VqdmirYnn0d{BxcG:|cHjvdplt[XSrb36gc4YheDdyU{\L NWXQSo95OjN6N{S4PFA>
LNCaP MnzCR4VtdCCYaXHibYxqfHliQYPzZZk> Mo\NNE0yOCEQvF2= NFHmR|EzPCCqwrC= MkjS[IVkemWjc3XzJINmdGxidnnhZoltcXS7IHnuJIEh\G:|ZTDk[ZBmdmSnboSgcYFvdmW{ M2riWlI{QDRyNkC1
PC-3 NFHUeJVE\WyuIG\pZYJqdGm2eTDBd5NigQ>? M2PHWFAuOTBizszN NVi1fG9[OjRiaNMg M{LYZ4Rm[3KnYYPld{Bk\WyuII\pZYJqdGm2eTDpckBiKGSxc3Wg[IVx\W6mZX70JI1idm6nch?= MnnPNlM5PDB4MEW=
MDA-MB-468  M4Tu[WNmdGxiVnnhZoltcXS7IFHzd4F6 NVTX[|RuOC1zMDFOwG0> MWWyOEBpyqB? MXfk[YNz\WG|ZYOgZ4VtdCC4aXHibYxqfHliaX6gZUBld3OnIHTldIVv\GWwdDDtZY5v\XJ? NGLmR4IzOzh2ME[wOS=>
LNCaP NGmxfVdHfW6ldHnvckBCe3OjeR?= Mn7ENlAx6oDVOECwJI5O MVKyOEBpyqB? NVLn[4JK\GWlcnXhd4V{KHSqZTDwbI9{eGixconsZZRqd25ibHX2[Ywhd2ZicEewV|ZMKGmwIHGg[I9{\SCmZYDlcoRmdnRibXHucoVz NX;SXXYzOjN6NEC2NFU>
PC-3 M3nSWmZ2dmO2aX;uJGF{e2G7 NV\rWJNjOjBy4pETPFAxKG6P NYPZW4Q{OjRiaNMg M{XOcIRm[3KnYYPld{B1cGVicHjvd5Bpd3K7bHH0bY9vKGyndnXsJI9nKHB5MGO2T{BqdiCjIHTvd4Uh\GWyZX7k[Y51KG2jbn7ldi=> MUiyN|g1ODZyNR?=
MDA-MB-468  M331SmZ2dmO2aX;uJGF{e2G7 M13PdVIxOOLCk{iwNEBvVQ>? NGHpW|AzPCCqwrC= MYLk[YNz\WG|ZYOgeIhmKHCqb4PwbI9zgWyjdHnvckBt\X[nbDDv[kBxPzCVNlugbY4h[SCmb4PlJIRmeGWwZHXueEBu[W6wZYK= MlznNlM5PDB4MEW=
Caki-1  NHfiZW1HfW6ldHnvckBCe3OjeR?= MVSxNFAuOjByMDDuUS=> MmTDNVAuOThyIH3pci=> NF7JN5BFVVOR NGPNSFRqdmirYnn0d{Bjd3SqIH3UU3JEOSCjbnSgcXRQWkN{IHHzJIlv\GmlYYTl[EBjgSC2aHWg[IVkemWjc3WgbY4heGixc4Doc5J6dGG2aX;uJI9nKGSxd37zeJJm[W1iZX\m[YN1d3K| MYOyN|M1QTl6OR?=
786-O MXjGeY5kfGmxbjDBd5NigQ>? MXGxNFAuOjByMDDuUS=> M1v4UVExNTF6MDDtbY4> M3HGXWROW09? MlHkbY5pcWKrdIOgZo91cCCvVF;SR|Eh[W6mIH3UU3JEOiCjczDpcoRq[2G2ZXSgZpkhfGinIHTlZ5Jm[XOnIHnuJJBpd3OyaH;yfYxifGmxbjDv[kBld3ewc4Ty[YFuKGWoZnXjeI9zew>? NHfQXYszOzN2OUm4PS=>
Caki-1  NWLQNoJMS2WubDDWbYFjcWyrdImgRZN{[Xl? MmnvN|AxNTRyMECgcm0> NYnFVZI{OjRvOU[gbC=> NXPabFBCTE2VTx?= MU\zeZBxemW|c3XzJJRp\SClZXzsJJZq[WKrbHn0fUBqdiCkb4ToJJRqdWViYX7kJIRwe2ViZHXw[Y5l\W62IH3hco5meg>? NWLKOppROjN|NEm5PFk>
786-O M2fFfmNmdGxiVnnhZoltcXS7IFHzd4F6 MYOzNFAuPDByMDDuUS=> NX\Ib3VYOjRvOU[gbC=> NV\YVpdbTE2VTx?= M3v2cpN2eHC{ZYPz[ZMhfGinIHPlcIwhfmmjYnnsbZR6KGmwIHLveIghfGmvZTDhcoQh\G:|ZTDk[ZBmdmSnboSgcYFvdmW{ NWfMWI9COjN|NEm5PFk>
Caki-1  Mn3vSpVv[3Srb36gRZN{[Xl? NWq5N3Z{OiEEtV2= NIfiPFY4OiCq NUXuOFZFTE2VTx?= NXq4Xo82cW6mdXPld{BIOSClZXzsJIN6[2ynIHHydoV{fCCjbnSgZZV1d3CqYXf5 NHjUc4ozOzN2OUm4PS=>
786-O MVnGeY5kfGmxbjDBd5NigQ>? M1PReFIhyrWP NXi1d3N5PzJiaB?= MWfEUXNQ NXHKdFhQcW6mdXPld{BIOSClZXzsJIN6[2ynIHHydoV{fCCjbnSgZZV1d3CqYXf5 M3nlcVI{OzR7OUi5

他の多くの細胞株試験データをご覧になる場合はこちらをクリックして下さい

アッセイ
Methods Test Index PMID
Western blot
p-S6K / S6K / p-4E-BP1 / E7 / E6 / p53 ; 

PubMed: 28115701     


Normoxic HPV-positive cancer cells were treated for 24 h with 0.5, 1.0, or 5 μM KU-0063794 (KU) or 50 nM rapamycin. Shown are immunoblots of P-S6K, S6K, P-4E-BP1, 4E-BP1, HPV16/18 E6/E7, and p53 protein levels. DMSO served as a solvent control; β-actin, as a loading control.

p-mTOR; 

PubMed: 24262658     


Inhibition of mTOR pathway by mTOR kinase inhibitors. MCC-2 cells were treated with WYE354 (3 μM), PP242 (2.5 μM), and Ku-0063794 (5 μM) for 24h, respectively. Lysates were prepared and subjected to immunoblotting analysis with indicated antibodies. 

28115701 24262658
体内試験 Ku0063794 inhibits tumor growth and mTOR signaling in a preclinical renal cell carcinoma model. However, Ku0063794 was not more effective than temsirolimus in the animal study. A possible explanation for lack of greater activity in vivo for Ku0063794 is that temsirolimus has important effects on the tumor microenvironment. Temsirolimus decreased angiogenesis in the xenograft tumors while Ku0063794 did not. Temsirolimus treated tumors expressed less VEGF and PDGF than Ku0063794 treated tumors, thus stimulating less angiogenesis[2].

お薦めの試験操作(参考用のみ)

キナーゼ試験:

[1]

- 合併

mTOR complexes kinase assays:

HEK-293 cells are freshly lysed in Hepes lysis buffer. Lysate (1-4 mg) is pre-cleared by incubating with 5-20 μL of Protein G-Sepharose conjugated to pre-immune IgG. The lysate extracts are then incubated with 5-20 μL of Protein G-Sepharose conjugated to 5-20 μg of either anti-Rictor or anti-Raptor antibody, or pre-immune IgG. All antibodies are covalently conjugated to Protein G-Sepharose. Immunoprecipitations are carried out for 1 hour at 4 °C on a vibrating platform. The immunoprecipitates are washed four times with Hepes lysis buffer, followed by two washes with Hepes kinase buffer. For Raptor immunoprecipitates used for phosphorylating S6K1, for the initial two wash steps the buffer includes 0.5 M NaCl to ensure optimal kinase activity. GST-Akt1 is isolated from serum-deprived HEK-293 cells incubated with PI-103 (1 μM for 1 hour). GST-S6K1 is purified from serum-deprived HEK-293 cells incubated with rapamycin (0.1 μM for 1 hour). mTOR reactions are initiated by adding 0.1 mM ATP and 10 mM MgCl2 in the presence of various concentrations of KU-0063794 and GST-Akt1 (0.5 μg) or GST-S6K1 (0.5 μg). Reaction are carried out for 30 minutes at 30 °C on a vibrating platform and stopped by addition of SDS sample buffer. Reaction mixtures are then filtered through a 0.22-μm-poresize Spin-X filter and samples are subjected to electrophoresis and immunoblot analysis with the indicated antibodies.
細胞試験:

[1]

- 合併
  • 細胞株: Wild-type and mLST8 deficient MEFs
  • 濃度: Dissolved in DMSO, final concentration ~3 μM
  • 反応時間: 24, 48, and 72 hours
  • 実験の流れ:

    Cells are treated with KU-0063794 for 24, 48, and 72 hours, and the medium is changed every 24 hours with freshly dissolved KU-0063794. For the measurement of cell growth, cells are washed once with PBS, and fixed in 4% (v/v) paraformaldehyde in PBS for 15 minutes. After washing once with water, the cells are stained with 0.1% Crystal Violet in 10% ethanol for 20 minutes and washed three times with water. Crystal Violet is extracted from cells with 0.5 mL of 10% (v/v) ethanoic (acetic) acid for 20 minutes. The eluate is then diluted 1:10 in water and absorbance at 590 nm is quantified. For the assessment of cell cycle distribution, cells are harvested by trypsinization, washed once in PBS, and re-suspended in ice-cold aq. 70% (v/v) ethanol. Cells are washed twice in PBS plus 1% (w/v) BSA and stained for 20 minutes in PBS plus 0.1% (v/v) Triton X-100 containing 50 g/mL propidium iodide and 50 g/mL RNase A. The DNA content of cells is determined using a FACSCalibur flow cytometer and CellQuest software. Red fluorescence (585 nm) is acquired on a linear scale, and pulse width analysis is used to exclude doublets. Cell-cycle distribution is determined using FlowJo software.


    (参考用のみ)
動物試験:

[2]

- 合併
  • 動物モデル: Nu/Nu nude mice
  • 投薬量: 8 mg/kg
  • 投与方法: i.p.
    (参考用のみ)

溶解度 (25°C)

体外 DMSO 16 mg/mL (34.36 mM)
Water Insoluble
Ethanol Insoluble
体内 左から(NMPから)右の順に溶剤を製品に加えます(文献ではなく、Selleckの実験によるデータ):
30% PEG400+0.5% Tween80+5% propylene glycol
混合させたのち直ちに使用することを推奨します。
30 mg/mL

* 溶解度測定はSelleck技術部門によって行われており、その他文献に示されている溶解度と差異がある可能性がありますが、同一ロットの生産工程で起きる正常な現象ですからご安心ください。

化学情報

分子量 465.54
化学式

C25H31N5O4

CAS No. 938440-64-3
Storage powder
in solvent
別名 N/A
Smiles COC1=C(CO)C=C(C=C1)C2=NC3=NC(=NC(=C3C=C2)N4CCOCC4)N5CC(C)OC(C)C5

投与溶媒組成計算器(クリア溶液)

ステップ1:実験データを入力してください。(実験操作によるロスを考慮し、動物数を1匹分多くして計算・調製することを推奨します)
投与量 mg/kg 動物平均体重 g 投与体積(動物毎) ul 動物数
ステップ2:投与溶媒の組成を入力してください。(ロット毎に適した溶解組成が異なる場合があります。詳細については弊社までお問い合わせください)
% DMSO % % Tween 80 % ddH2O
計算リセット

便利ツール

モル濃度計算器

モル濃度計算器

求めたい質量、体積または濃度を計算してください。

質量 (mg) = 濃度 (mM) x 体積 (mL) x 分子量 (g/mol)

モル濃度計算器方程式

  • 質量
    濃度
    体積
    分子量

*貯蔵液を準備するとき、常に、オンであるとわかる製品のバッチに特有の分子量を使って、を通してラベルとMSDS/COA(製品ページで利用可能な)。

希釈計算器

希釈計算器

貯蔵液を準備するために必要な希釈率を計算してください。Selleck希釈計算器は、以下の方程式に基づきます:

開始濃度 x 開始体積 = 最終濃度 x 最終体積

希釈の計算式

この方程式は、一般に略語を使われます:C1V1 = C2V2 ( 入力 出力 )

  • C1
    V1
    C2
    V2

常に貯蔵液を準備するとき、小びんラベルとMSDS/COA(オンラインで利用できる)で見つかる製品のバッチに特有の分子量を使ってください。

連続希釈計算器方程式

  • 連続希釈剤

  • 計算結果

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):
分子量計算器

分子量计算器

そのモル質量と元素組成を計算するために、合成物の化学式を入力してください:

総分子量:g/mol

チップス: 化学式は大文字と小文字の区別ができます。C10H16N2O2 c10h16n2o2

モル濃度計算器

質量 濃度 体積 分子量

技術サポート

ストックの作り方、阻害剤の保管方法、細胞実験や動物実験の際に注意すべき点など、製品を取扱う時に問い合わせが多かった質問に対しては取扱説明書でお答えしています。

Handling Instructions

他に質問がある場合は、お気軽にお問い合わせください。

  • * 必須

mTORシグナル伝達経路

mTOR Inhibitors with Unique Features

相関mTOR製品

Tags: KU-0063794を買う | KU-0063794 ic50 | KU-0063794供給者 | KU-0063794を購入する | KU-0063794費用 | KU-0063794生産者 | オーダーKU-0063794 | KU-0063794化学構造 | KU-0063794分子量 | KU-0063794代理店
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細胞株 試験類型 濃度 培養時間 溶剤類型 活性叙述 PMID